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Purity: ≥98%
Decription: AMBMP (also known as BML-284; BML284) is a novel, potent and cell-permeable Wnt signaling activator with anti-inflammatory activity. AMBMP induces TCF-dependent transcriptional activity(EC50 =700 nM).
| Targets |
TCF-dependent transcriptional activity (EC50 = 700 nM)
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|---|---|
| ln Vitro |
The migration and invasion capacities of MNK45 and AGS cells are markedly enhanced by BML-284 (10 μM; 24 hours), while the migration and invasion capacities of cells blocked by pizotifen are partially restored [1]. When compared to the NC group, BML-284 (10 μM; 24 h) dramatically increased the expression of β-catenin. Additionally, as compared to the pizotifen treatment group, it partially counteracted the effects of pizotifen on the expression of N- and E-cadherin in MNK45 and AGS cells [1].
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| ln Vivo |
In a study where Tg (myl7:EGFP) transgenic embryos at 5.5 hpf were placed into cells with 20 embryos on a plate, BML-284 (10 ng) and pyrimethanil (4 mg/L) together partially prevented the teratogenic phenotype and heart abnormalities produced by pyrimethanil[1].
AMBMP Targets CaMKIIβ In Vivo, https://pmc.ncbi.nlm.nih.gov/articles/PMC7659555/ Researchers next asked whether AMBMP acts by enhancing CaMKIIβ activity in vivo. C3KO and C57BL/6 WT mice were treated with AMBMP and then their muscles were evaluated for CaMKIIβ and other signaling pathways. The activation of signaling was carried out by western blotting with antibodies specific for the active forms of these signaling pathways. Treatment with AMBMP (daily i.p. injection 7.5 mg/kg) led to CaMKIIβ activation in both WT and C3KO mice (Figures 4C and 4D). The drug appears to engage CaMKIIβ specifically as it does not activate AKT nor AMPK (nor other pathways that control muscle remodeling and oxidative metabolism) (Figures 4E and 4F). Furthermore, the effect of AMBMP on CaMKIIβ was likely post-transcriptional, and there was no significant change in the expression level of the Camk2b gene (Figure 4G). Thus, these studies establish proof of concept for the ability of AMBMP to activate CaMKII and subsequently to promote oxidative metabolism and benefit the LGMDR1 phenotype. |
| Cell Assay |
Western Blot Analysis[2]
Cell Types: Human gastric cancer cell lines MNK45 and AGS[1] Tested Concentrations: 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: β-catenin expression was induced in MNK45 and AGS and E-cadherin and N-cadherin expressing cells were retained . |
| Animal Protocol |
Compound pharmacokinetics assay
For pharmacokinetics, AMBMP was administered by different routes of delivery (subcutaneous, intraperitoneal, and oral, in food or by gavage) at two different dosages (10 mg/kg and 30 mg/kg). The blood was collected at 0.5 h, 1 h, 2 h, 4 h and 6 h post treatment by heart puncture. The concentrations of compounds in plasma were analyzed by Integrated Analytical Solutions, Inc.https://pmc.ncbi.nlm.nih.gov/articles/PMC7659555/ Seahorse analysis of Extracts from Frozen Muscle For Seahorse analysis, frozen soleus muscles from DMSO or AMBMP-treated mice (daily IP injections at 7.5 mg/kg) were homogenized by hand in a Dounce homogenizer in 200 mL of mitochondrial buffer (70 mM sucrose, 220 mM mannitol, 5 mM KH2PO4, 5 mM MgCl2, 1 mM EGTA, 2 mM HEPES, adjusted to pH 7.4 with KOH) on ice. Muscle homogenates were centrifuged at 900xg for 5 min at 4°C. Supernatants were transferred to new tubes; protein concentrations were measured using BCA protein Assay Kit. The samples (4 μg/well) were analyzed in the UCLA Mitochondrial and Metabolism Core using a Seahorse XF96 Analyzer. Data were normalized to total protein. Seahorse analysis was carried out according to Acin-Perez et al.https://pmc.ncbi.nlm.nih.gov/articles/PMC7659555/ |
| References |
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| Additional Infomation |
N4-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine is a member of pyrimidines.
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| Molecular Formula |
C19H19CLN4O3
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|---|---|
| Molecular Weight |
350.37
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| Exact Mass |
350.137
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| Elemental Analysis |
C, 65.13; H, 5.18; N, 15.99; O, 13.70
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| CAS # |
853220-52-7
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| Related CAS # |
BML-284 hydrochloride;2095432-75-8
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| PubChem CID |
11210285
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
623.4±65.0 °C at 760 mmHg
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| Flash Point |
330.8±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
3.72
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
455
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C(NCC2C=C3C(OCO3)=CC=2)=CC(C2C=C(OC)C=CC=2)=NC=1N
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| InChi Key |
FABQUVYDAXWUQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N4O3/c1-24-14-4-2-3-13(8-14)15-9-18(23-19(20)22-15)21-10-12-5-6-16-17(7-12)26-11-25-16/h2-9H,10-11H2,1H3,(H3,20,21,22,23)
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| Chemical Name |
C19H18N4O3
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| Synonyms |
AMBMP; BML284; BML 284; BML-284; Wnt Agonist
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~285.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8541 mL | 14.2706 mL | 28.5413 mL | |
| 5 mM | 0.5708 mL | 2.8541 mL | 5.7083 mL | |
| 10 mM | 0.2854 mL | 1.4271 mL | 2.8541 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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